Biological Activity
Originally defined as a selective inhibitor of ATR and ATM kinases. Induces cell death in prematurely senescent breast cancer cells. Decreases p21CIP1 levels in premature senescent MCF-7 and HCT-116 cells; also exhibits antiproliferative activity in a range of cancer cell lines. Blocks camptothecin-induced p53 phosphorylation and protects cells from camptothecin-induced apoptosis.
Compound Libraries
CGK 733 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 555.84 |
| Formula | C23H18Cl3FN4O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 905973-89-9 |
| PubChem ID | 6605258 |
| InChI Key | HLCDNLNLQNYZTK-UHFFFAOYSA-N |
| Smiles | [O-][N+](=O)C1=CC(NC(=S)NC(NC(=O)C(C2=CC=CC=C2)C2=CC=CC=C2)C(Cl)(Cl)Cl)=CC=C1F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| DMSO | 55.58 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 555.84. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 1 mM | 1.8 mL | 9 mL | 17.99 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.6 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.8 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDSReferences
References are publications that support the products\' biological activity.
Crescenzi et al (2008) Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: Implications for chemotherapy. Clin.Cancer Res. 14 1877 PMID: 18347191
Bhattacharya et al (2009) Role of polyamines in p53-dependent apoptosis of intestinal epithelial cells. Cell Signal. 21 509 PMID: 19136059
Alao and Sunnerhagen (2009) The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation. Radiat.Oncol. 10 4 PMID: 19903334
Won et al (2008) Retraction: small molecule-based reversible reprogramming of cellular lifespan. Nat.Chem.Biol. 4 431 PMID: 18560433
Keywords: CGK 733, supplier, CGK733, p21, antiproliferative, p53, Other, Apoptosis, Other, Apoptosis, Tocris Bioscience
